|MZP-55|CsnPharm

CAS No.: 2010159-48-3

MZP-55 Catalog No. CSN21379

MZP-55 is a VHL-based PROTAC targeting on BET with pDC₅₀/D_max (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032.

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描述MZP-55 is a VHL-based PROTAC targeting on BET with pDC₅₀/D_max (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032. MZP-55 at concentration ranging in 30-1000nM led a dose-dependent degradation of BRD3,4, as well as slight degradation of BRD2, in HeLa cells post 24-hour treatment. MZP-55 at concentration of 50nM achieved a depletion of BRD4 by 81% and downregulation of c-MYC, the target of BRD4, by 60% in MV4;11 cells treated for 4h. Also it exhibited anti-proliferation of MV4;11 and HL60 cells with _pEC₅₀/E_max (%) values of 7.08/96.4 and 6.37/98.3, respectively, post 48h^[1].
参考文献

[1] Chan KH, Zengerle M, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.9253 mL
- 4.6265 mL
- 9.2531 mL
- 5 mM
- 0.1851 mL
- 0.9253 mL
- 1.8506 mL
- 10 mM
- 0.0925 mL
- 0.4627 mL
- 0.9253 mL

技术信息

CAS号	2010159-48-3	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C57H70ClN7O10S	运输	蓝冰
分子量	1080.72	别名

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